Introduction

Uses for Fluorides

Dental Caries

Prevent or reduce the incidence of dental caries; slow or reverse the progression of existing dental lesions.107109bdeijstv

Effect of fluoride is predominantly posteruptive; maintain consistent small amounts of fluoride in saliva and dental plaque.109113 (See Actions.)

As a dietary supplement for the prevention of dental caries in children in areas where the concentration of fluoride ion in drinking water is less than optimal.109

American Dental Association (ADA) recommends that all patients, including those without dental caries and with no apparent increased risk of dental caries, receive adequate water fluoridation or oral fluoride supplementation, combined with daily use of fluoridated dentifrice and twice-yearly topical application of fluoride.128

CDC supports fluoridation of the public water supply as the most cost-effective means of providing optimal levels of fluoride to large segments of the population.109

Optimal concentration of fluoride ion in drinking water is approximately 1 ppm (range 0.7–1.2 ppm), depending on the annual mean maximum daily temperature of the area.106109bw In warm climates where more water is likely to be ingested, concentrations should be at the lower end of the range.106109

In communities where the concentration of fluoride in the water supply is >2 ppm, use an alternative source of drinking water for children ≤8 years of age.109

Because consumption of commercially available beverages (including bottled water) in the US and Canada is displacing the consumption of tap or well water, the relative importance of fluoridation of local community water on fluoride intake may be affected.107 However, current recommendations in children continue to be based on the fluoride concentrations in local drinking water.106107

ADA and others recommend that in areas where oral fluoride supplements are necessary, children 6 months to 16 years of age receive daily fluoride supplements to provide maximum benefit to both deciduous and permanent teeth.a

Efficacy of topically applied fluoride varies according to the concentration of fluoride ion in the preparation, method and frequency of application, and the duration of use.a

Acidulated phosphate fluoride gels (alone or in combination with a saliva substitute) have been used to control dental decay after xerostomia-producing radiation therapy of tumors of the head and neck.a

Stannous fluoride gels have been used to prevent decalcification in orthodontic patients.a

Stannous fluoride gels have been used to protect against postirradiation caries.a

Desensitizing Dentin

Bone Diseases

Has been used to increase bone density and relieve bone pain in the treatment of various metabolic and neoplastic bone diseases†.a

Has been used in conjunction with calcium and vitamin D or calcium and estrogen to reduce skeletal fracture rates in osteoporosis†; further study is needed.a

Has been used alone or in conjunction with calcium carbonate as an adjunct in the management of bone lesions in multiple myeloma†.a

Has been used to reduce bone pain in metastatic prostatic carcinoma†.a

Has been reported to stabilize the progression of hearing loss in a limited number of patients with otosclerosis†.a

Has been used to increase spinal (but not femoral neck) bone mineral density (BMD) in corticosteroid-induced osteoporosis†;108 however, further studies are needed and other therapies are preferred.108

Fluorides Dosage and Administration

Administration

Administer orally as a lozenge, solution, or chewable tablet or topically as a cream, dentifrice, foam, gel, rinsing solution, or solution.aehlopsv

Oral Administration

Administer sodium fluoride orally as a lozenge, chewable tablet, or as a solution undiluted or mixed with juice or water.b Dissolve chewable tablets in the mouth or chew before swallowing, preferably at bedtime after brushing the teeth.abj

Administer oral fluoride supplements only when community fluoridation programs are not available or feasible and when the fluoride ion concentration in drinking water is ≤0.6 ppm (mg/L).a

Oral Topical Administration

Rinsing solution may be swallowed only if directed to do so by a clinician to provide systemic fluoride supplementation.103

To minimize the amount of fluoride swallowed and absorbed systemically and the risk of fluorosis, instruct and/or supervise children <12 years of age regarding proper techniques for use of topical preparations.100101103i (See Dental Fluorosis under Cautions.)

For maximum benefit, do not eat or drink for ≥30 minutes after administration; adults, do not rinse mouth for 30 minutes after administration.119121ademnostv

5% solution: May be applied by dental personnel to moist teeth.h Apply to teeth with cotton swabs, brush, or probe.h Do not dry.h Patient should not eat hard foods or brush for ≥2 hours after application.h Avoid other fluoride preparations on the day of application.h Suspend use of fluoride tablets for several days after treatment.h

Foam or 1.23% gel: Dental personnel may apply after prophylaxis.ot Prior to filling mouth trays, shake foam bottle vigorously for 3–4 seconds.o Have patient bite down lightly on mouth tray(s) for 1–4 minutes.ot Remove tray(s) and have patient expectorate excess.ot Gel may also be applied by swab.t

For desensitizing exposed root surfaces, use gel after brushing and flossing at bedtime.a

Oral Topical Administration (Stannous Fluoride)

0.4% gel: After brushing teeth normally, shake toothbrush to remove excess water; apply the gel to cover the bristles.l Brush teeth thoroughly; allow the gel to remain on the teeth for 1 minute, then expectorate.124125l For sensitivity relief, use a toothbrush or cotton swab to ensure that all sensitive areas are covered with the gel.124125l

0.1% rinsing solution: Dilute before use.i Use after regular brushing and flossing.117118i Swish vigorously around and between teeth for 1 minute; expectorate.117118i Repeat.117118i

For home irrigators, pour 30 mL of the diluted 0.1% solution into the irrigator reservoir; add 120 mL of water and mix thoroughly to provide a 0.02% stannous fluoride rinse.i Consult the manufacturer’s prescribing information for additional information on preparation and use of the concentrated solution with home irrigators.117118i

Dosage

Available as sodium fluoride, acidulated phosphate fluoride, sodium monofluorophosphate, or stannous fluoride; dosage expressed in terms of the fluoride ion.acijnop

Dosage of oral fluoride supplements varies according to the age of the child and the concentration of fluoride in the drinking water.109110 Adjust dosage in proportion to the amount of fluoride provided from all possible sources (e.g., childcare settings, school, bottled water, dentifrice, multivitamins, mouth rinse).a109110 Do not exceed recommended dosages.a (See Dental Fluorosis and also see Pediatric Use under Cautions.)

Fluoride Supplementation in Areas with Insufficient Fluoride in Drinking Water

Oral

Table 2. Oral Daily Dosage of Supplemental Fluoride (as Lozenge, Chewable Tablet, or Solution) for Children Living in Areas with Insufficient Fluoride in Drinking Water (Expressed in Terms of Fluoride Ion)106107109jw

Fluoride Ion Concentration in Drinking Water

Age

<0.3 ppm

0.3–0.6 ppm

>0.6 ppm

0 to <6 months

None

None

None

6 months to <3 years

0.25 mg

None

None

3 to <6 years

0.5 mg

0.25 mg

None

6–16 years

1 mg

0.5 mg

None

Sodium Fluoride

Oral Topical

1.1% cream in children ≥6 years of age: Brush for 2 minutes once daily, preferably at bedtime.121de

1.1% gel in children ≥6 years of age: Once daily, preferably at bedtime.119s

0.044 or 0.05% rinsing solution in children ≥6 years of age: 10 mL once daily at bedtime.116np

0.2% rinsing solution in children ≥6 years of age: 10 mL once weekly, preferably at bedtime.115m

Acidulated Phosphate Fluoride

Oral Topical

1.1% gel in children ≥6 years of age: Once daily, preferably at bedtime.v

1.2 or 1.23% foam or 1.23% gel in children ≥6 years of age: Apply once every 6–12 months.ao In patients with rampant or active caries, may repeat 1–2 times every 6 months.ao

Stannous Fluoride

0.1% rinsing solution in children ≥12 years of age: Dilute before use to a 0.1% solution.i (See Dilution under Dosage and Administration.) Use 15 mL once daily.117118i Repeat with an additional 15 mL.117118i May use more frequently as directed by clinician.i

Stannous Fluoride

0.1% rinsing solution: Dilute before use to a 0.1% solution.i (See Dilution under Dosage and Administration.) Use 15 mL once daily.117118i Repeat with an additional 15 mL.117118i May use more frequently, as directed by clinician.i

Warnings/Precautions

Warnings

Dental Fluorosis

Excessive amounts may produce dose-related dental fluorosis (hypocalcification and hypoplasia) and osseous changes in children <8 years of age, especially where water fluoridation >0.6 ppm.107abdefijmosv

Mild fluorosis has no effect on tooth function; may render the enamel more resistant to caries.107 May cause white opaque patches on the incisal edges of anterior teeth or cusp tips of posterior teeth (“snow capping”).107

Skeletal Fluorosis

Prolonged intake of high fluoride ion concentrations (i.e., 4–8 ppm [mg/L]) in drinking water may result in an increase in bone mineral density and apparent fluoride osteosclerosis.107 Risk of developing fluorosis directly related to the extent and duration of fluoride exposure; crippling skeletal fluorosis is extremely rare in the US.107

Teeth Surface and Restoration Staining

Staining or pigmentation (e.g., yellow, brown, brown-black) of the teeth may result from topical application of concentrated solutions or gels of stannous fluoride, particularly in patients with poor oral hygiene.ai Good oral hygiene (e.g., adequate brushing) minimizes risk of staining; staining is not harmful or permanent and can be removed by dentist.103i

Sensitivity Reactions

Allergic Reactions

Urticaria, exfoliative dermatitis, atopic dermatitis, stomatitis, and GI and respiratory allergic reactions have occurred rarely following the use of dentifrices or multivitamin preparations containing fluoride.ah

Patients with mucositis or with abraded or sensitive gingival tissue may be hypersensitive to alcohol or other ingredients contained in some oral or topical fluoride preparations.afmov

General Precautions

Use of Fixed Combinations

When fluoride is used in fixed combination with other preparations, consider the cautions, precautions, and contraindications associated with the concomitant agent(s).a (See Pediatric Use under Cautions.)

Specific Populations

Pregnancy

The ADA currently does not recommend fluoride supplements during pregnancy.a

Lactation

Distributed into milk in small amounts.a Use with caution in nursing women.fijmosv

Pediatric Use

ADA, American Academy of Pediatric Dentistry (AAPD), and AAP currently do not recommend oral fluoride supplements in infants <6 months of age.106107j

In children <2 years of age, consider other sources of fluoride when weighing the risks and benefits of using fluoridated dentifrice.109

Instruct and/or supervise children 2–12 years of age carefully regarding the proper use of topical fluoride-containing products to minimize repeated swallowing and the risk of dental fluorosis.100101103eimsv

Efficacy of oral fluoride supplements in controlling dental caries in children >16 years of age not established.109

Sodium fluoride chewable tablets: Safety and efficacy not established in children <6 months of age.j

Sodium fluoride 1.1% topical cream, gel, and rinsing solution: Safety and efficacy not established in children <6 years of age.demns

Acidulated phosphate fluoride topical foam and gel: Safety and efficacy not established in children <6 years of age.ov

Stannous fluoride oral rinsing solutions and topical gels: Safety and efficacy not established in children <12 years of age.117118124125i

May be difficult to appropriately adjust the amount of fluoride required from fixed-combination multivitamin or multivitamin/iron preparations used as oral fluoride supplements.a (See Dosage in Dosage and Administration.)

Geriatric Use

No overall differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.fmo Substantially eliminated by the kidneys; geriatric patients more likely to have decreased renal function; monitor renal function and adjust dosage accordingly.fmo

Renal Impairment

Excreted by the kidney; therefore, risk of toxic reactions may be greater in patients with impaired renal function.fmo

Fluorides Pharmacokinetics

Absorption

Bioavailability

Sodium fluoride and other soluble fluoride salts: Readily and almost completely absorbed from the GI tract.107ab

≥80% of soluble fluoride probably absorbed from the GI tract in the absence of high dietary concentrations of calcium or certain other cations.107 (See Interactions.)

Food

Milk, infant formula, or certain foods (e.g., with high concentrations of calcium or certain other divalent or trivalent cations that form insoluble fluoride salts) may decrease absorption of fluoride by 10–25%.107

Distribution

Extent

Crosses the placenta and is distributed in small amounts into milk, sweat, tears, and hair.a

Elimination

Elimination Route

Rapidly excreted principally in urine, and in small amounts in feces, sweat, and saliva.ab

Special Populations

Hemodialysis may remove fluoride in patients with severe intoxication or with impaired renal function.a

Stability

Storage

Oral

Solution

Sodium fluoride: Tight, plastic containers at <40°C (maintain between 15–30°C), especially if the pH of the solution is <7.5.a May decompose and become alkaline when stored in ordinary pharmaceutical glass.ab Store and dispense in plastic, paraffin-lined flasks or USP type 1 borosilicate glass containers.b

Prior to tooth eruption, fluoride is incorporated into tooth enamel during formation.a

Cariostatic effects on teeth after eruption result from combined effects of bacterial metabolism in plaque and on the dynamics of enamel demineralization and remineralization during an acidogenic challenge.107

Increases skeletal density and bone mass; however, large doses can cause skeletal fluorosis and osteomalacia.a

Advice to Patients

Advise patients receiving fluoride powders or concentrated rinsing solutions that the preparation must be reconstituted and/or diluted as directed prior to use.103i

Advise patients receiving fluoride treatment gels or rinsing solutions for self-administration that these preparations are to be used as directed and not as dentifrices or mouthwashes or gargles, respectively.103i

Advise individuals receiving stannous fluoride-containing preparations of the importance of good oral hygiene (e.g., adequate brushing) to minimize the risk of staining.103i Inform patients that such staining is not harmful or permanent and can be removed by a dentist or dental hygienist.103i

Instruct and/or supervise children <12 years of age during use of topical fluoride preparations (e.g., rinsing solutions, gels, dentifrices) to minimize the risk of fluorosis and the amount of fluoride swallowed and absorbed systemically.100101103i Instruct children, especially those 2–6 years of age, not to swallow topical fluoride products.100101109 Inform individuals with children that ingestion of higher than recommended levels of fluoride by children has been associated with an increase in mild dental fluorosis in developing, unerupted teeth.w

Importance of long-term compliance on a daily basis in patients who require oral fluoride supplements.w

Advise patients not to brush or eat hard foods for 2 hours after application of topical solution.h

Advise patients to contact a poison control center or other qualified clinician immediately if they swallow more fluoride than the amount used for brushing or rinsing.ln

Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.bcdefijlmnopstwvh

Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.bcdefijlmnopstwvh

Importance of informing patients of other important precautionary information.bcdefijlmnopstwvh (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

108. American College of Rheumatology Task Force on Osteoporosis Guidelines. Recommendations for the prevention and treatment of glucocorticoid-induced osteoporosis. Arthritis Rheumatism. 1996; 39:1791-801. http://www.ncbi.nlm.nih.gov/pubmed/8912500?dopt=AbstractPlus

109. Centers for Disease Control and Prevention. Recommendations for using fluoride to prevent and control dental caries in the United States. MMWR Morb Mortal Wkly Rep. 2001; 50(No. RR-14):1-42. http://www.ncbi.nlm.nih.gov/pubmed/11215787?dopt=AbstractPlus http://www.cdc.gov/mmwr/PDF/rr/rr5014.pdf